GSK 2833503A

Pricing Availability   Qty
Description: Potent and selective TRPC6 and TRPC3 antagonist
Chemical Name: [2-[(4-Chloro-2-fluorophenyl)amino]-5-methyl-4-thiazolyl][(2S,3S)-2,3-dimethyl-1-piperidinyl]methanone
Purity: ≥98% (HPLC)
Citations (1)

Biological Activity for GSK 2833503A

GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cells in vitro and in cardiomyocytes.

Compound Libraries for GSK 2833503A

GSK 2833503A is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for GSK 2833503A

M. Wt 381.89
Formula C18H21ClFN3OS
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1366234-01-6
PubChem ID 71818575
Smiles C[C@H]1CCCN(C(C2=C(SC(NC3=C(C=C(C=C3)Cl)F)=N2)C)=O)[C@H]1C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for GSK 2833503A

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 38.19 100
ethanol 7.64 20

Preparing Stock Solutions for GSK 2833503A

The following data is based on the product molecular weight 381.89. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.62 mL 13.09 mL 26.19 mL
5 mM 0.52 mL 2.62 mL 5.24 mL
10 mM 0.26 mL 1.31 mL 2.62 mL
50 mM 0.05 mL 0.26 mL 0.52 mL

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References for GSK 2833503A

References are publications that support the biological activity of the product.

Washburn et al (2013) The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore. Bioorg.Med.Chem.Lett. 23 4979 PMID: 23886683

Seo et al (2014) Combined TRPC3 and TRPC6 blockade by selective small-molecule or genetic deletion inhibits pathological cardiac hypertrophy. Proc.Natl.Acad.Sci.U.S.A. 111 1551 PMID: 24453217

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Keywords: GSK 2833503A, GSK 2833503A supplier, GSK2833503A, GSK503A, TRPC3, TRPC6, transient, receptor, potential, canonical, channel, anatagonists, potent, selective, TRPC, 6497, Tocris Bioscience

1 Citation for GSK 2833503A

Citations are publications that use Tocris products. Selected citations for GSK 2833503A include:

Jonathan H et al (2022) Genetic- and diet-induced ω-3 fatty acid enrichment enhances TRPV4-mediated vasodilation in mice. Cell Rep 40 111306 PMID: 36070688

Do you know of a great paper that uses GSK 2833503A from Tocris? Please let us know.

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